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黑色素纳米粒的电响应控制药物释放。

Electro-responsive controlled drug delivery from melanin nanoparticles.

机构信息

I3B's Research Institute on Biomaterials Biodegradables and Biomimetics, Universidade do Minho, Headquarters of the European Institute of Excellence on Tissue Engineering and Regenerative Medicine, Barco, Guimarães, Portugal; ICVS/3B's - PT Government Associated Laboratory, Braga, Guimarães, Portugal.

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal; REQUIMTE/LAQV, Group of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal.

出版信息

Int J Pharm. 2020 Oct 15;588:119773. doi: 10.1016/j.ijpharm.2020.119773. Epub 2020 Aug 15.

Abstract

Electro-responsive controlled drug delivery has been receiving an increasing interest as one of the on-demand drug delivery systems, aiming the improvement of the therapeutics efficacy by controlling the amount of drug release at a specific time and target site. Herein, we report a simple method to develop an electro-responsive controlled drug delivery system using functionalized melanin nanoparticles (FMNPs) with polydopamine and polypyrrole to precisely control the release of dexamethasone (Dex). Optimized FMNPs showed 376.77 ± 62.05 nm of particle size, a polydispersity index of 0.26 ± 0.09 and a zeta-potential (ZP) of -32.59 ± 3.61 mV. FMNPs evidenced a spherical shape, which was confirmed by scanning electron microscopy. Fourier-transform infrared spectrometry analysis confirmed the deposition of the polymers on the FMNPs' surface. The incorporation efficiency of the optimized Dex-loaded FMNPs was 94.45 ± 0.63% and the increase of ZP to -40.34 ± 4.65 mV was attributed to the anionic nature of Dex. In vitro Dex release studies without stimuli revealed a maximum Dex release below 10%. Applying electrical stimulation, Dex release was augmented, with a maximum of ca. 32% after 24 h. The designed FMNPs provide a powerful biomaterial-based technological tool for electro-responsive controlled drug delivery, capable of surpassing the associated lack of efficiency and stability of current carriers.

摘要

电响应控制药物递送作为一种按需药物递送系统,受到越来越多的关注,旨在通过在特定时间和靶位控制药物释放量来提高治疗效果。在此,我们报告了一种使用具有聚多巴胺和聚吡咯的功能化黑色素纳米粒子(FMNPs)来开发电响应控制药物递送系统的简单方法,以精确控制地塞米松(Dex)的释放。优化后的 FMNPs 粒径为 376.77±62.05nm,多分散指数为 0.26±0.09,zeta 电位(ZP)为-32.59±3.61mV。FMNPs 呈球形,这通过扫描电子显微镜得到了证实。傅里叶变换红外光谱分析证实了聚合物在 FMNPs 表面的沉积。优化的载 Dex FMNPs 的包封效率为 94.45±0.63%,ZP 增加到-40.34±4.65mV,这归因于 Dex 的阴离子性质。在没有刺激的情况下进行的体外 Dex 释放研究表明,最大 Dex 释放低于 10%。施加电刺激后,Dex 的释放增加,24 小时后最大释放约为 32%。设计的 FMNPs 为电响应控制药物递送提供了一种强大的基于生物材料的技术工具,能够克服当前载体效率和稳定性方面的不足。

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